KR20200090818A - Mpges-1 억제제로서의 신규 화합물 - Google Patents

Mpges-1 억제제로서의 신규 화합물 Download PDF

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Publication number
KR20200090818A
KR20200090818A KR1020207017202A KR20207017202A KR20200090818A KR 20200090818 A KR20200090818 A KR 20200090818A KR 1020207017202 A KR1020207017202 A KR 1020207017202A KR 20207017202 A KR20207017202 A KR 20207017202A KR 20200090818 A KR20200090818 A KR 20200090818A
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pain
compound
linker
disease
mpges
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Ceased
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KR1020207017202A
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Korean (ko)
Inventor
요하네스 알베르투스 마리아 스메이틴크
줄리엔 데이비드 비야스
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콘드리온 아이피 비.브이.
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Priority to KR1020257022058A priority Critical patent/KR20250109241A/ko
Publication of KR20200090818A publication Critical patent/KR20200090818A/ko
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/66—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355—Tocopherols, e.g. vitamin E
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4462—Non condensed piperidines, e.g. piperocaine only substituted in position 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020207017202A 2017-11-22 2018-11-22 Mpges-1 억제제로서의 신규 화합물 Ceased KR20200090818A (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020257022058A KR20250109241A (ko) 2017-11-22 2018-11-22 Mpges-1 억제제로서의 화합물

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17203033 2017-11-22
EP17203033.0 2017-11-22
PCT/EP2018/082146 WO2019101826A1 (en) 2017-11-22 2018-11-22 Compounds as mpges-1 inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020257022058A Division KR20250109241A (ko) 2017-11-22 2018-11-22 Mpges-1 억제제로서의 화합물

Publications (1)

Publication Number Publication Date
KR20200090818A true KR20200090818A (ko) 2020-07-29

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Family Applications (2)

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KR1020207017202A Ceased KR20200090818A (ko) 2017-11-22 2018-11-22 Mpges-1 억제제로서의 신규 화합물
KR1020257022058A Pending KR20250109241A (ko) 2017-11-22 2018-11-22 Mpges-1 억제제로서의 화합물

Family Applications After (1)

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KR1020257022058A Pending KR20250109241A (ko) 2017-11-22 2018-11-22 Mpges-1 억제제로서의 화합물

Country Status (16)

Country Link
US (1) US11672787B2 (pl)
EP (1) EP3713564B1 (pl)
JP (2) JP7754623B2 (pl)
KR (2) KR20200090818A (pl)
CN (1) CN111417393A (pl)
AU (1) AU2018371153B2 (pl)
BR (1) BR112020010089A2 (pl)
CA (1) CA3079483A1 (pl)
ES (1) ES2963906T3 (pl)
IL (1) IL274821A (pl)
MX (1) MX2020005238A (pl)
MY (1) MY207603A (pl)
PL (1) PL3713564T3 (pl)
SG (1) SG11202003743SA (pl)
WO (1) WO2019101826A1 (pl)
ZA (1) ZA202002103B (pl)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102660473B1 (ko) * 2017-04-05 2024-04-24 콘드리온 아이피 비.브이. 미토콘드리아 질환의 신규 치료
NL2024431B1 (en) * 2019-12-11 2021-09-07 Sulfateq Bv Compounds for treatment of alzheimer’s disease
NL2025730B1 (en) * 2020-06-02 2022-01-20 Sulfateq Bv Compounds for treatment of sepsis
WO2025242849A1 (en) * 2024-05-24 2025-11-27 Khondrion Ip B.V. Chromanyl derivatives for use in the treatment of bone disorders

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JPH02250831A (ja) * 1989-03-23 1990-10-08 Kuraray Co Ltd ３，４―ジヒドロ―２ｈ―ベンゾピラン誘導体及びそれを有効成分とする抗消化性潰瘍剤
US7442716B2 (en) 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
AU2005316091B2 (en) 2004-12-17 2011-12-01 Merck Canada Inc. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-D]imidazoles as mPGES-1 inhibitors
DE102006053475A1 (de) 2006-11-14 2008-06-19 Eberhard-Karls-Universität Tübingen Zubereitungen zur Hemmung der Prostaglandin E2 Synthese
DE102006058450A1 (de) 2006-12-12 2008-06-19 Eberhard-Karls-Universität Tübingen Zubereitungen zur Hemmung der Prostaglandin E2 Synthese
WO2009061744A2 (en) 2007-11-06 2009-05-14 Edison Pharmaceuticals, Inc. 4- (p-quinonyl)-2-hydroxybutanamide derivatives for treatment of mitochondrial diseases
WO2009130242A1 (en) 2008-04-23 2009-10-29 Novasaid Ab Low molecular weight derivatives and use thereof in treatment of prostaglandin e synthase related diseases
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UY32138A (es) 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
UY32470A (es) 2009-03-05 2010-10-29 Boehringer Ingelheim Int Derivados de 2-{2-cloro-5-[(sustituido) metil]fenilamino} -1-metil]fenilamino}-1-metilbencimidazol-5-carboxamidas-n-(sustituidas) y sus sales fisiológicamente aceptables, composiciones conteniéndolos y aplicaciones
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WO2013153535A1 (en) 2012-04-13 2013-10-17 Glenmark Pharmaceuticals S.A. TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
HUE033757T2 (en) 2012-07-12 2017-12-28 Khondrion Ip B V Chromanyl derivatives for treating mitochondrial disease
HRP20170532T4 (hr) * 2012-07-12 2019-12-27 Khondrion Ip B.V. Derivati kromanila za liječenje mitohondrijske bolesti
NL2010010C2 (en) 2012-12-19 2014-06-23 Sulfateq B V Compounds for protection of cells.
PT3133068T (pt) 2014-04-14 2021-01-06 Shanghai hengrui pharmaceutical co ltd Derivados de amida e sais farmacêuticos destes, método de preparação destes e aplicação medicinal destes
NL2013012B1 (en) * 2014-06-17 2016-07-05 Sulfateq Bv Compounds for the treatment of chronic obstructive airway diseases.
ES2927699T3 (es) * 2015-05-22 2022-11-10 Sulfateq Bv Compuesto para la profilaxis o el tratamiento de nefropatía diabética o enfermedad renal diabética
ES3033538T3 (en) 2015-10-08 2025-08-05 Khondrion Ip B V Novel compounds for treating mitochondrial disease
KR102660473B1 (ko) * 2017-04-05 2024-04-24 콘드리온 아이피 비.브이. 미토콘드리아 질환의 신규 치료
EP3713563B1 (en) * 2017-11-22 2025-02-19 Khondrion Ip B.V. Amide derivatives of chromanyl or chromanyl quinones for use in treating depression and migraine

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EP3713564C0 (en) 2023-11-15
CN111417393A (zh) 2020-07-14
JP2021504307A (ja) 2021-02-15
MY207603A (en) 2025-03-06
IL274821A (en) 2020-07-30
US20200345706A1 (en) 2020-11-05
KR20250109241A (ko) 2025-07-16
ZA202002103B (en) 2023-12-20
MX2020005238A (es) 2020-08-24
CA3079483A1 (en) 2019-05-31
BR112020010089A2 (pt) 2020-11-03
JP7754623B2 (ja) 2025-10-15
EP3713564B1 (en) 2023-11-15
US11672787B2 (en) 2023-06-13
AU2018371153B2 (en) 2023-07-13
WO2019101826A1 (en) 2019-05-31
ES2963906T3 (es) 2024-04-03
PL3713564T3 (pl) 2024-04-08
RU2020120235A (ru) 2021-12-22
AU2018371153A1 (en) 2020-06-04
EP3713564A1 (en) 2020-09-30
SG11202003743SA (en) 2020-06-29
JP2024009799A (ja) 2024-01-23

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